Pycnogenol (PYC) is a plant-based extract derived from the proprietary bark of the French maritime pine (Pinus pinaster ssp. atlantica) that exerts antioxidative, anti-inflammatory, and anti-platelet effects. The standardized extract is composed of phenolic compounds (catechin, epicatechin, and taxifolin), condensed flavonoids (classed as procyanidins/ proanthocyanidins) and phenolic acids (cinnamic acids and other glycosides). these phenolic compounds after being ingested, undergo biotransformation and are broken down in the colon by microbial enzymes yielding smaller, bioavailable molecules that can then be absorbed by the colon into the bloodstream and transported to tissues and organs. The pycnogenol possess a highly protective characteristics versus various cardiovascular dysfunctions, kidney diseases, hepatic dysfunctions, neuro cognitive disorder, diabetes, reproductive dysfunction and infertility, cancer, digestive, retinal disease. The present review illustrates the effect of Pycnogenol as antioxidant and anti-inflammatory effects along with anti-tumor influence as well. Pycnogenol was concluded to act as an antioxidant agent in different situation including heart stress, cardiovascular system abnormalities, kidney disease and hepatic disorders, so it can be used in combination with other medication such as Methotrexate to abolish its side effects.